CAS: 1672665-49-4; (S)-3-((2,2-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1H-Inden-4-yl)Oxy)-5-Fluorobenzonitrile

📜4-(甲硫基)苯酚置于oxone,Noyori'S Catalyst,甲酸,草酰氯,Caesium Carbonate,Sodium Sulfate,Selectfluor,三乙胺,N,N-二甲基甲酰胺,三氟乙酸,Magnesium Chloride体系中,用 环丁砜,二氯甲烷,N,N-二甲基乙酰胺,水,乙腈,仲丁醇,苯 用作溶剂,化学反应 57.0H,反应生成(S)-3-(((2,2-二氟-1-羟基-7-(甲基磺酰基)-2,3-二氢-1H-茚满-4-基)氧基)-5-氟苄腈
参考文献: Hif-2α Inhibitors For Treating Iron Overload Disorders[fr] Inhibitors Hif-2α Pour Traiter Des Troubles D'Hémochromatose
标题: Hif-2α Inhibitors For Treating Iron Overload Disorders[fr] Inhibitors Hif-2α Pour Traiter Des Troubles D'Hémochromatose
摘要:本公开涉及hif-2α抑制剂及其制备和用于治疗铁过载疾病的方法.某些化合物在hif-2α闪烁近距离法,荧光素酶法和vegf Elisa法中表现出很强的活性,并且在预防和治疗小鼠模型中减少了肝铁积累和血清铁参数.

专利信息

专利号:US-2021190788-A1
优先权日:2019-12-19
标 题 :PET RADIOPHARMACEUTICALS FOR NON-INVASIVE EVALUATION OF HIF-2alpha
发明人：BRUGAROLAS JAMES; SUN XIANKAI; DEBNATH SASHI
权利人:UNIV TEXAS
摘要:Provided herein are hypoxia inducible factor 2-alpha (HIF-2α)-specific radioactive tracers, methods of use thereof, and methods of synthesis thereof. Specifically, provided herein are HIF-2α-specific radioactive tracers comprising an HIF-2α-specific agent developed as a therapeutic inhibitor and a positron emitting radioactive label. Embodiments provide methods of detecting an HIF-2α-expressing tumor, detecting an HIF-2α inhibitor resistant tumor, evaluating a change in HIF-2α expression in response to an anti-cancer treatment, detecting acquisition of HIF-2α inhibitor resistance, evaluating efficacy of an HIF-2α depletion therapy, or detecting or monitoring an ischemic area in a subject. Also provided are methods of synthesizing an HIF-2α-specific radioactive tracer.

专利号:US-2021187130-A1
优先权日:2019-12-19
标题 :PET RADIOPHARMACEUTICALS FOR NON-INVASIVE EVALUATION OF HIF-2alpha
发明人：BRUGAROLAS JAMES; SUN XIANKAI; DEBNATH SASHI
权利人:UNIV TEXAS
摘要:Provided herein are hypoxia inducible factor 2-alpha (HIF-2α)-specific radioactive tracers, methods of use thereof, and methods of synthesis thereof. Specifically, provided herein are HIF-2α-specific radioactive tracers comprising an HIF-2α-specific agent developed as a therapeutic inhibitor and a positron emitting radioactive label. Embodiments provide methods of detecting an HIF-2α-expressing tumor, detecting an HIF-2α inhibitor resistant tumor, evaluating a change in HIF-2α expression in response to an anti-cancer treatment, detecting acquisition of HIF-2α inhibitor resistance, evaluating efficacy of an HIF-2α depletion therapy, detecting or monitoring an ischemic area in a subject, or detecting and monitoring pulmonary hypertension in a subject. Also provided are methods of synthesizing an HIF-2α-specific radioactive tracer.

专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.